Ralinepag is a cyclohexyl amide derivative patented by Arena Pharmaceuticals, Inc. as agonists of the human prostacyclin (PGI2) receptor useful for the treatment of pulmonary arterial hypertension. Ralinepag shows selectivity in both binding and functional assays with respect to most members of the prostanoid receptor family and a more modest 30-50-fold selectivity over the EP3 receptor. Ralinepag had an excellent PK profile across species. Enterohepatic recirculation most probably contributes to a concentration-time profile after oral administration in the cynomolgus monkey that showed a very low peak-to-trough ratio. Phase III clinical trial is currently ongoing.

N-Methyl-D-aspartic acid is an amino acid derivative acting as a specific agonist at the NMDA receptor, and therefore mimics the action of the neurotransmitter glutamate on that receptor. Unlike glutamate, NMDA only binds to and regulates the NMDA receptor and has no effect on other glutamate receptors (such as those for AMPA and kainate). NMDA receptors are particularly important when they become overactive during withdrawal from alcohol as this causes symptoms such as agitation and, sometimes, epileptiform seizures. NMDA is a water-soluble synthetic substance that is not normally found in biological tissue.

COTI-2 is an orally available small molecule targeting p53, a tumor suppressor gene that is mutated in over 50% of all cancers. The drug was developed by Clinical Outcome Technologies Inc (now Cotinga Pharmaceuticals) and is believed to act by reactivating mutant p53 and inhibiting the phosphatidylinositol 3-kinase (PI3K)/Akt. The drug is being evaluated in phase I clinical trials for the treatment of gynecologic cancers and head and neck squamous cell carcinoma.

DL-Kynurenine is a racemic mixture of D-kynurenine and L-kynurenine. Kynurenine is the precursor of kynurenic acid, an endogenous antagonist of the glycine site of the NMDA (N-methyl-D-aspartate) receptor. Kynurenine has been identified as an endogenous ligand of the aryl hydrocarbon receptor (AhR), a receptor known to be activated by various environmental toxicants, such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD).

Scopafungin (also known as GE4800) is an inhibitor of oxidative phosphorylation in mitochondria. Scopafungin also inhibits, in vitro, a variety of pathogenic fungi, yeasts, and gram-positive bacteria.

Metindizate was developed as a spasmolytic agent. Information about the current use of this compound is not available.

Ruzasvir (previously known as MK-8408) was developed as a nonstructural protein 5A (NS5A) inhibitor for the treatment of hepatitis C and hepatitis C infection. Ruzasvir successfully completed phase II clinical trial for combination therapy. The obtained results have shown that ruzasvir in combination with uprifosbuvir was highly effective and well-tolerated in participants infected with hepatitis C virus genotypes GT1, GT2, GT4, GT5, and GT6, with a lower efficacy in GT3-infected persons.